摘要
以相同的肝微粒体温孵体系对（＋）－和（－）－黄皮酰胺（Ｃｌａ）进行了温孵，以ＨＰＬＣ分析比较了代谢结果，发现（＋）－和（－）－Ｃｌａ所产生的主要代谢产物基本相同，但主要代谢产物在（＋）－和（－）－Ｃｌａ温孵体系中含量差别较大，左旋体代谢产生的ＣＭ１和ＣＭ５的量比右旋体大；ＣＭ２是左旋Ｃｌａ的主要代谢产物之一，右旋体产生极小的量；而ＣＭ３是右旋Ｃｌａ的主要代谢产物，左旋体产生的量较少．ＣＭ４，ＣＭ６是由ＣＭ３进一步代谢所产生的双羟基代谢产物，右旋体产生的量多于左旋体．定量分析（＋）－，（－）－Ｃｌａ在肝微粒体中不同时间的代谢情况，发现（＋）－，（－）－Ｃｌａ在实验浓度下均为非线性动力学，二者代谢速率基本相同，不同时间代谢的立体选择性基本相同．
The metabolic differences between (+) and (-) clausenamide in rat liver microsomes were found by comparing their metabolites. The (-) clausenmide generates more CM1 and CM5 than the (+) clausenamide. CM2 is one of the main metabolites of (-) clausenamide but only minor was detected in (+) clausenamide incubate. The amount of CM3 generated from (+) clausenamide is much more than from (-) clausenamide. The (+) clausenamide produces more CM4 and CM6 than the (-) clausenamide. By quantitative analysis of the amount of (+) and (-) clausenamide metabolized in rat liver microsomes at different times, it was found that the pharmacokinetics of both (+) and (-) clausenamide were non linear.
出处
《中国药理学与毒理学杂志》
CAS
CSCD
北大核心
1999年第3期214-216,共3页
Chinese Journal of Pharmacology and Toxicology
关键词
黄皮酰胺
微粒体
生物转化
立体选择性
clausenamide
microsome
biotransformation
stereoselectivity
